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‫ض ظَ ْه َر َك* َو َرفَ ْعنَا َل َك ِذ ْك َر َك*‬‫نك ِوز َْر َك* ا ‪8‬ل ِذي أَن َق َ‬‫ض ْعنَا َع َ‬ ‫ش َر ْح َل َك َ‬
‫ص ْد َر َك* َو َو َ‬ ‫)أ َ َل ْم نَ ْ‬ ‫
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‫ار َغب(‪.‬‬ ‫ب* َو إِ َلى َرب‪َ D‬ك فَ ْ‬ ‫س ًرا* فَ ِإذَا فَ َر ْغتَ فَ َ‬
‫انص ْ‬ ‫س ًرا* إِ ‪8‬ن َمعَ ا ْل ُع ْ‬
‫س ِر يُ ْ‬ ‫س ِر يُ ْ‬‫فَ ِإ ‪8‬ن َمعَ ا ْل ُع ْ‬ ‫
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‬ ‫‪Introduction to‬‬
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‬ ‫‪Pharmacokinetics‬‬
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‬ ‫‪DR. ABDULHADI BURZANGI / DR. MAHA JAMAL‬‬
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‬ ‫‪PHARMACOLOGY DEPARTMENT‬‬
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‫‪COLLEGE OF MEDICINE‬‬
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Objectives:

By the end of the lecture, you should be able to:

1. Identify key terms that determine drug

pharmacokinetics

2. List factors affecting absorption & distribution

3. Describe phases of drug metabolism and

841160 6

factors affecting microsomal enzyme activity

4. Mention the routes of drug excretion

Pharmacokinetics

• Pharmacokinetics is defined as the study

of the bodily processes that affect the

movement of a drug in the body.

(what the body does to a drug?)

• The major processes involved in

pharmacokinetics are Absorption,

Distribution, Metabolism, and Excretion

(referred to collectively as ADME a i

processes).

Absorption

circulation 3 s G I gabsorptioy.b.Drugoraa.bld.ie

• Absorption is the transfer of a drug from its site of administration to the

bloodstream.

word
• Factors Affecting Absorption as o (patient-specific factors)

• Blood Circulation: A patient who is in shock or cardiopulmonary arrest will need to
means

a have medications administered intravenously to achieve the desired response
xnxx.si i

iesimi na because of the reduced blood circulation in these situations.

• Contact time with the epithelial lining of the GI tract:. In people with a very rapid transit

www.wa.no time through the GI tract, due to severe diarrhea for example, medication cannot be
surmises.at effectively absorbed.
e
www.aol.o.me
wet

• Drug-food or drug-drug interactions with other compounds present in the GI tract:
giessen so Specific foods or other drugs may bind a drug and prevent absorption. The interaction

iwate
mum between tetracycline and dairy products or antacids is a good example of this effect.

semen

say w y
has
antibiotics

a so.ie! xi enter acion ‫بيعمل‬

‫لبان تحتوي ع كالسيوم‬Z‫مع اي من منتجات ا‬
tetracycline ‫متصاص في‬Z‫تمنع ا‬

# " ‫يد سورييي‬c‫أخيرا احس هرجة كثير في ذي الس‬$

ً ‫ مع الحليب‬tetracycline ‫الزبده ماراح اخذ‬

Absorption

Factors affecting absorption : (Drug-specific factors)

Ø Route of administration. www.swi.ua
oasis tie

Ø Dosage forms (depending on particle size and disintegration, ease of dissolution).

D iscsi> a
(solution suspension > capsule > atablet)

sis miss

Ø Molecular weight of drug: Diffusion is most efficient with drugs that are small molecules.
sissies

W Ø Lipid solubility: Drugs, which are usually somewhat lipid-soluble (fat-soluble), readily
a
sissies as move across most biological membranes.

Estee
www.msn.si osa

Ø Degreewww.iw.no aim gammas.ws eisxis s
sims form is absorbable.
of ionization: Only unionized

F mm
Ø Drug solubility (aqueous preparation better than oily, suspension preparations)

 Bioavailability and First-Pass Effect

• The bioavailability of a drug is the fraction (F) of the

administered dose that reaches the systemic
circulation.
IV
• Bioavailability is defined as unity (or 100%) in the case of
intravenous administration.
• For a drug administered orally, bioavailability may be less
than 100% for two main reasons: incomplete extent of
absorption across the gut wall and first-pass effect by the
liver.
• First-pass effect (presystemic elimination) is defined as
the elimination of drug that occurs after administration
but before it enters the systemic circulation. (eg, during
passage through the gut wall, portal circulation, or liver
for an orally administered drug)
 ‫جمعنا الدواء في الدورة الدموية‬
1-Absorption:We collected the drug in the circulatory system

‫عضاء‬5‫ نحتاج إلى توصيله إلى ا‬، ‫بعد أن يدخل الدواء الدورة الدموية‬
2-Distribution: After the drug enters the blood circulation, we need to deliver it to the organs

Distribution

Distribution is the process by which a drug is carried to sites of action throughout the

body by the blood- stream.

The delivery of a drug from the bloodstream to the site of drug action primarily
depends on blood as.me
flow, capillary permeability, the degree of binding (attachment)

of the drug to blood and tissue proteins, and the relative lipid-solubility of the drug

molecule. enosorugsolubiloses
absorption andDistribution

Factors Affecting Distribution

i
fa.TT
• Binding to plasma proteins (Albumin) affects drug distribution into tissues, because only drug that

is not bound is available to penetrate tissues, bind to receptors, and exert activity.

• Body composition

• Cardiac decompensation (heart failure).

• Age of the patient.
These factors all affect the apparent volumesaints
t.wis.jo
of distribution (Vd) of a drug and ultimately play a role

in determining the appropriate dose of a drug.

Distribution

id e s ebeimi gavolume
Volume of distribution (Vd) is the hypothetical o asI needed to account for all of the drug

in the am isso
body based on the serum concentration in a blood sample.

: ‫ الدكتورة مها‬-

! ‫ت مو معانا‬/‫عاد‬1‫ا‬

:‫الطالبات‬-

a

Phastaciton

Metabolism or Biotransformation

• Metabolism is a process by which drugs may undergo chemical changes that allow them
3

mean to be more easily excreted.

goosrausmananoristration
I

ers.noorn.es • There are two types of metabolic processes drugs undergo in the liver.

• In the first type of reaction, drugs are made more polar through oxidation-reduction
1
seas enzymes, most often those of
carentainsission reactions or hydrolysis. These reactions use metabolic

so the cytochrome P450 enzyme system, to catalyze the biotransformation.
52

omom• The second type of metabolism involves conjugation reactions. In this type of reaction,

the drug is joined with another substance, such as glucuronic acid, sulfuric acid, acetic

acid, or an amino acid. Glucuronidation is the most common conjugation reaction.

The result of conjugation is a more water-soluble compound that is easier for the

kidneys to excrete.

noooo

8in
a Phase I Phase II my
ojos

E Drug Metabolite
Conjugated

not aw Oxidation conjugation Drug

Reduction reactions
Hydrolysis

Elimination

• The complete removal of the drug from the body is referred to

as Elimination. Elimination of drug from the body may involve

C
processes occurring in the kidney, z
the lung, s
the liver, and other

Iorg.am
stfm organs. iminatnn
• Excretion into the urine is one of the most important

mechanisms of drug removal.

• Clearance (CL) relates the rate of elimination to the plasma

F concentration.

• Clearance depends on the drug, blood flow, and the

condition of the organs of elimination in the patient

Half Life (t1/2)

Pharmacokinetic

• Half-life (t1/2) is the time required for the

amount of drug in the body or blood to fall

by 50%.

• Half-life (t1/2) will depend on both the

volume of distribution and the clearance:

x X

• The half-life determines the rate at which

blood concentration rises during a constant

infusion and falls after administration is

‫ ومن التشتت وضعف التركيز‬،‫اللهم إنّي أعوذ بك من نسيان ما درست‬

stopped.

.‫ يضيع منها شيء‬J‫ يتف ّلت و‬L‫علومات في عقلي ف‬P‫أن تُثبّت ا‬ ‫ي‬J‫ وأسألك يا مو‬،‫والقلق‬

Pharmacokinetic Video

I Wilsow a 0

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